黄芩素A环的结构修饰

Structural Modification of the A-ring Baicalein

以传统中药黄芩的主要活性成分黄芩苷及其乙酰化产物6,7-二乙酰氧基黄芩素为原料,通过碘代、硝化及硝基还原胺化反应在A环的C-8上引入碘原子、硝基及胺基,并对黄芩素A环上的3个酚羟基进行了选择性二甲醚化及全甲醚化,制备了A环修饰的6种黄芩素衍生物,表征了它们的结构,讨论了合成方法的特点。

Using baicalin,the main active component of a traditional Chinese herb Scutellaria baicalensis, and one of its derivative,6,7-diacetoxylbaicalein,as precursors,a series of C8-substituted and di or tri-O-methylated baicalein derivatives was synthesized in good yields by iodination,nitration,reductive amination and selective methoxylation or hydrolysis of 6,7-diacetoxylbaicalein.The structures of these producrs were characterized.They featured with a broad spectrum of biological activities,notably anti-oxidant.